BTRX-335140

BTRX-335140 is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. BTRX-335140 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) . BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats.